Phenolic Alkaloids Of Menispermum Dauricum Transdermal Drug Delivery In Vitro

Objective: PAMD is commonly used in Chinese medicine Menispermaceae from plant roots to extract the menispermum dauricum DC various chemical structure similar to a mixture of fat-soluble alkaloids, mainly composed of dauricine. With blood circulation, promoting qi movement and relieving pain, expansion of coronary vessels, improve myocardial ischemia, for the prevention and treatment of coronary heart disease, arrhythmia, angina, and bleeding resistance of the Chest, dizziness, shortness of breath, palpitations, chest tightness or pain disorders . Nowadays, only regular oral tablets, capsules, injection and other formulations of use. According to physical and chemical properties dauricine, and cardiovascular disease requires long-term drug use characteristics, this article will be developed into cataplasms to enable it to avoid the liver first pass effect and gastrointestinal drug degradation; a long time of drug administration can enter the body at a constant rate, reducing delivery times, and extend the dosing interval; to maintain a stable blood concentration, reduce its toxicity side effects; easy to use, can be interrupted at any time delivery, especially for patients should not be taken orally.Method: The modified Franz diffusion cell study, the main experimental device, the skin of rabbit for the transdermal diffusion, determined by HPLC sampling points were calculated cumulative permeation amount Q value to Q-t equation and the penetration rate constant J for evaluation, transdermal diffusion filter dauricine the best receiver solution, the best penetration enhancers, Orthogonal experimental design, appropriate choice of matrix and the best preparation, preparation of the best dauricine cataplasms. Conducted on dauricine cataplasms product quality and safety evaluation in vitro.Result: The comparison of Q-t equation and transdermal speed constant showed that pH5.8 phosphate buffer solution- saline was the best for the study;3% Azone as skin permeation enhancers better;the best ratio of matrix is Gelatin: D-sorbitol: Ca(OH)2 : PANa : PVP-K30 : CMC-Na : Kaolin : propanedione : glycerol : PEG 400 =4:20:0.15:1: 7: 4: 4: 3.5: 4: 10. The best preparation is to obtain prescriptions, said additional amount of water soaked gelatin swelled by adding D-sorbitol, Ca (OH) 2, dauricine raw material medicine, the swelling water bath was I phase solution; for an alternative PANa, PVP-K30, CMC-Na, kaolin, propanedione, glycerol, PEG 400 were mixed overnight swelling may beⅡphase solution; I phase andⅡphase solution was mixed; the last to join Azone to mix a few minutes to paste uniform, smooth, may contain drug cataplasms; will evenly coated on the non-woven on the matrix, 50℃bake 90min, covered with anti-sticking layer, sealed packaging.Conclusion: This method is simple and easy, stability, controllability, good repetition.